US5026857AExpiredUtility

Substituted basic 2-aminotetralin in pharmaceuticals

68
Assignee: BAYER AGPriority: Dec 10, 1986Filed: Jul 12, 1989Granted: Jun 25, 1991
Est. expiryDec 10, 2006(expired)· nominal 20-yr term from priority
C07D 211/58C07D 285/14C07D 209/44C07D 275/06C07C 255/00C07D 453/02C07D 279/02C07C 2603/74C07C 233/62C07D 213/82C07D 211/88C07D 209/16C07D 209/14C07D 209/48C07D 295/096C07D 275/02C07D 471/10C07D 211/26
68
PatentIndex Score
5
Cited by
9
References
8
Claims

Abstract

For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R 1 represents hydrogen or alkyl, R 2 represents hydrogen, alkyl or acyl, and R 3 represents quinuclidine or a group of the formula --(CH 2 ) a --R 4 , --CH 2 --CH═CH--(CH 2 ) b --R 4 , --CH 2 C.tbd.C--(CH 2 ) b --R 4 , ##STR2## wherein a denotes a number from 1 to 10, b denotes a number 0, 1, 2, 3 or 4, c denotes a number 0, 1 or 2, d denotes a number 2 or 3, and x denotes oxygen, sulphur or NR 5 , and their salts.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
       1. A substituted basic 2-aminotetralin of the formula ##STR124## wherein R 1  represents hydrogen or lower alkyl, R 2  represents hydrogen, lower alkyl, lower alkylcarbonyl, or benzoyl,   c denotes a number 0, 1 or 2,   d denotes a number 2 or 3,   X denotes oxygen or the group NR 5 , where     R 5  represents hydrogen, or represents lower alkyl which is optionally substituted by hydroxyl or amino, or represents phenyl, benzyl, lower alkoxycarbonyl, lower alkylsulphonyl or carbamoyl,   
     
     
       2. A substituted basic 2-aminotetralin or salt according to claim 1, wherein R 1  represents hydrogen or methyl,   R 2  represents hydrogen, methyl, ethyl, propyl, isopropyl, acetyl or propionyl,   c denotes a number 1 to 2,   d denotes the number 2,   X denotes the NR 5  group, where     R 5  represents hydrogen, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, phenyl, benzyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl, methylsulphenyl, ethylsulphonyl or carbamoyl.   
     
     
       3. A compound according to claim 1, wherein such compound is 2-(1-ethoxycarbonypiperidin-4-yl-)amino-8-methoxy-1,2,3,4-tetrahydronaphthalene of the formula ##STR125## or its salt. 
     
     
       4. A compound according to claim 1, wherein such compound is 8-methoxy-2-(1-methylpiperidin-4-yl-)amino-1,2,3,4-tetrahydronaphthalene of the formula ##STR126## or its salt. 
     
     
       5. A composition for treatment of a disorder of the central nervous system comprising an amount effective therefor of a compound or salt according to claim 1 and a physiologically acceptable diluent. 
     
     
       6. A unit dose of of a composition according to claim 5 in the form of a tablet, ampule or capsule. 
     
     
       7. A method of treating a patient suffering from a disorder of the central nervous system caused by a disturbance of the serotoninergic system, which comprises administering to such patient an amount effective therefor of a compound or salt according to claim 16.     
     
     
       8. The method according to claim 7, wherein such compound is 2-(1-ethoxycarbonypiperidin-4-yl-)amino-8-methoxy-1,2,3,4-tetrahydronaphthalene, and   8-methoxy-2-(1-methylpiperidin-4-yl-)amino-1,2,3,4-tetrahydronaphthalene, or its salt.

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